CN1195745C - 抗病毒大环化合物 - Google Patents
抗病毒大环化合物 Download PDFInfo
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- CN1195745C CN1195745C CNB998082600A CN99808260A CN1195745C CN 1195745 C CN1195745 C CN 1195745C CN B998082600 A CNB998082600 A CN B998082600A CN 99808260 A CN99808260 A CN 99808260A CN 1195745 C CN1195745 C CN 1195745C
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- phenylene
- carbon
- methylene radical
- pyridine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/06—Peri-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Ceramic Engineering (AREA)
- Manufacturing & Machinery (AREA)
- Virology (AREA)
- Oncology (AREA)
- Materials Engineering (AREA)
- Structural Engineering (AREA)
- Communicable Diseases (AREA)
- Inorganic Chemistry (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- AIDS & HIV (AREA)
- Cardiology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
表1 | ||||
抗HIV活性数据 | ||||
化合物 | CC50(ug/mL) | EC50(ug/mL) | SI | |
HIV-1(IIIB) | HIV-2 | HIV-1 | ||
1 AMD3465 | >250 | 0.008 | 0.032 | 3×104 |
2 AMD3538 | 209 | 0.1 | 6.7 | 2.0×103 |
3 AMD3500 | >250 | 0.6 | 10.3 | 417 |
4 AMD3499 | >250 | 1.8 | 28.5 | 138 |
5 AMD3498 | >250 | 0.2 | 7.1 | 1.2×103 |
6 AMD3497 | >250 | 1.8 | 3.8 | 138 |
7 AMD3516 | 158 | 0.7 | 9.8 | 225 |
8 AMD3530 | 175 | 0.5 | 2.0 | 350 |
9 AMD3517 | 153 | 0.8 | 10.6 | 191 |
10 AMD3544 | 222 | 0.7 | 3.7 | 317 |
11 AMD3543 | 239 | 0.2 | 1.0 | 1×103 |
12 AMD3529 | 130 | 0.4 | 2.6 | 325 |
化合物 | 对mAb 12G5结合的抑制IC50 a(ng/ml) |
AMD3100 | 27 |
AMD3465 | 3 |
AMD7049 | 52 |
AMD7050 | 1 |
AMD7051 | 7 |
AMD7058 | >1000 |
AMD7059 | >1000 |
AMD7063 | 9 |
SDF-1αb | 270 |
化合物 | %对Ca2+流动(浓度)或IC50 a(ng/ml)的抑制 |
AMD3100 | 5 |
AMD3465 | 1 |
AMD7049 | 100%(1μg/ml) |
AMD7050 | 100%(1μg/ml) |
AMD7051 | 100%(1μg/ml) |
AMD7058 | 44%(1μg/ml) |
AMD7059 | 36%(1μg/ml) |
AMD7063 | 100%(1μg/ml) |
化合物 | IC50 a(μg/mL) |
AMD3451 | 8.9 |
AMD3472 | 45.4 |
AMD3454 | 32.3 |
AMD3526 | 82 |
AMD3100 | >100 |
Claims (20)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US09/111,895 US6506770B1 (en) | 1996-06-06 | 1998-07-08 | Antiviral compounds |
US09/111,895 | 1998-07-08 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB2005100094866A Division CN100339080C (zh) | 1998-07-08 | 1999-07-08 | 抗病毒大环化合物 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1308617A CN1308617A (zh) | 2001-08-15 |
CN1195745C true CN1195745C (zh) | 2005-04-06 |
Family
ID=22341015
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB998082600A Expired - Fee Related CN1195745C (zh) | 1998-07-08 | 1999-07-08 | 抗病毒大环化合物 |
CNB2005100094866A Expired - Lifetime CN100339080C (zh) | 1998-07-08 | 1999-07-08 | 抗病毒大环化合物 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB2005100094866A Expired - Lifetime CN100339080C (zh) | 1998-07-08 | 1999-07-08 | 抗病毒大环化合物 |
Country Status (17)
Country | Link |
---|---|
US (6) | US6506770B1 (zh) |
EP (1) | EP1095031B1 (zh) |
JP (1) | JP4637353B2 (zh) |
KR (1) | KR100778134B1 (zh) |
CN (2) | CN1195745C (zh) |
AP (1) | AP1436A (zh) |
AU (1) | AU767359B2 (zh) |
BR (1) | BR9912524A (zh) |
CA (1) | CA2336634C (zh) |
HU (1) | HUP0102930A3 (zh) |
IL (1) | IL140605A0 (zh) |
MX (1) | MXPA01000137A (zh) |
NO (1) | NO20010047L (zh) |
NZ (1) | NZ509699A (zh) |
PL (1) | PL345516A1 (zh) |
TR (1) | TR200100030T2 (zh) |
WO (1) | WO2000002870A1 (zh) |
Families Citing this family (70)
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US6506770B1 (en) | 1996-06-06 | 2003-01-14 | Anormed, Inc. | Antiviral compounds |
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JP2004508421A (ja) * | 2000-09-15 | 2004-03-18 | アノーメッド インコーポレイティド | ケモカインレセプター結合性ヘテロ環式化合物 |
US7052676B2 (en) * | 2000-09-26 | 2006-05-30 | The Regents Of The University Of Michigan | Methods for inhibition of HIV replication using a small molecule inhibitor |
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RU2420284C2 (ru) * | 2006-06-12 | 2011-06-10 | Пфайзер Продактс Инк. | Антагонист ccr5 для усиления иммуновосстановительной терапии и лечения оппортунистической инфекции у пациентов с вич |
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WO2000009152A1 (en) | 1998-08-14 | 2000-02-24 | The University Of British Columbia | Therapeutic chemokine receptor antagonists |
JP2002506830A (ja) | 1998-03-13 | 2002-03-05 | ザ ユニバーシティ オブ ブリティッシュ コロンビア | 治療的ケモカイン受容体アンタゴニスト |
WO1999048528A1 (fr) | 1998-03-24 | 1999-09-30 | Chugai Seiyaku Kabushiki Kaisha | Inhibiteurs de vascularisation |
WO1999065507A1 (en) | 1998-06-19 | 1999-12-23 | The General Hospital Corporation | Modulating platelet function |
AU5241099A (en) * | 1998-07-31 | 2000-02-21 | Trustees Of Columbia University In The City Of New York, The | Use of inhibitors of the activation of cxcr4 receptor by sdf-1 in treating rheumatoid arthritis |
US6365583B1 (en) | 1999-02-02 | 2002-04-02 | Anormed, Inc. | Methods to enhance white blood cell count |
WO2005002522A2 (en) | 2003-06-30 | 2005-01-13 | Caritas St. Elizabeth's Medical Center Of Boston, Inc. | Compositions and methods for treating tissue ischemia |
US7315917B2 (en) * | 2005-01-20 | 2008-01-01 | Sandisk Corporation | Scheduling of housekeeping operations in flash memory systems |
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1998
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